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5-Ht3 Receptor Antagonists
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A kind of technology of CR5 and compound, applied in the field of 5-HT3 receptor antagonist
Active Publication Date: 2017-03-08
TAKEDA PHARMA CO LTD
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Summary
Abstract
Description
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Application Information
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Problems solved by technology
[0005] 5-HT3 antagonists currently on the market are only approved for the treatment of vomiting or irritable bowel syndrome
Method used
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Embodiment approach (A
[0062] In one embodiment, the compound of formula (I) as defined in the Summary, or a pharmaceutical salt thereof, is wherein Z is O.
Embodiment approach (B
[0064] In one embodiment, the compound of formula (I) or a pharmaceutical salt thereof as defined in the Summary is wherein Z is NR a . Within this embodiment, in another group of compounds, R a is hydrogen. Within this embodiment, in another group of compounds, R a is methyl.
[0065] Implementation plan (C)
[0066] In another embodiment, a compound of formula (I) or a pharmaceutical salt thereof as defined in the general and above embodiments (A) and (B) and groups contained therein, in a group of compounds, R 1 is a ring with the formula
[0067]
[0068] (a) Within the group in embodiment (C), in a group of compounds, R 1 is a ring of formula (a) or (d). Within (a), in one embodiment, R 1 is a ring with the formula
[0069]
[0070] (b) Within the group of embodiments (C), in another group of compounds, R 1 is a ring of formula (e), (f) or (g). In (b), in a group of compounds, R 1 is a ring of formula (e). In (b), in a group of compounds, R 1 is a ring...
Embodiment approach (D
[0078] In another embodiment, in a group of compounds, a compound of formula (I) or a pharmaceutical salt thereof as defined in the summary and above in embodiments (A) and (B) and groups contained therein is wherein R 1 is a ring with the formula
[0079]
[0080] (a1) Within the group in embodiment (D), in a group of compounds, R 1 is a ring of formula (c) or (h). Within this embodiment, in a group of compounds, the stereochemistry at the chiral carbon is (R) or (S).
[0081] (b1) Within the group in embodiment (D), in a group of compounds, R 1 is a ring of formula (b).
[0082] (vi) In embodiment (D) and groups of embodiments contained therein (ie (a1) and (b1) and groups contained therein), in a group of compounds each R 3 are independently hydrogen or methyl. Within these groups of compounds, in a group of compounds, each R 3 is hydrogen.
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Abstract
The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drugaddiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Description
[0001] This application is a divisional application of the patent application with the application number 201380045326.X, the application date is July 16, 2013, and the invention name is "5-HT3 receptorantagonist". technical field [0002] The present invention provides compounds that are 5-HT3 receptor antagonists and are therefore useful in the treatment of diseases treatable by inhibition of 5-HT3 receptors, such as emesis, pain, drugaddiction, neurodegenerative and psychiatric disorders and GI disorders. Also provided are pharmaceutical compositions containing the compounds and methods for preparing the compounds. Background technique [0003] The serotonin type 3 (5-HT3) receptor is part of the serotonergic system. Unlike the other receptors of this system, which are all G protein-coupled receptors, the 5-HT3 receptor is a ligand-gated ion channel and belongs to the superfamily of Cys-loop receptors, which Including nicotinic acetylcholine receptors, gamma-aminobuty...
Claims
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Application Information
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